2377335-74-3
2377335-74-3 structure
- Name: M-808
- Chemical Name: M-808
- CAS Number: 2377335-74-3
- Molecular Formula: C45H63FN6O5S
- Molecular Weight: 819.08
- Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
- Create Date: 2020-08-08 15:18:48
- Modify Date: 2024-01-09 15:36:46
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M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with a binding IC50 value of 2.6 nM[1].
| Name | M-808 |
|---|
| Description | M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with a binding IC50 value of 2.6 nM[1]. |
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| Related Catalog | |
| Target |
IC50: 1 nM (Menin-MLL in MV4;11 cells), 4 nM (Menin-MLL in MOLM-13 cells)[1]. |
| In Vitro | M808 exhibits IC50 values of 1 nM, 4 nM and 2.8 nM in MV4;11 cells, MOLM-13 cells and HL60 cells, respectively[1]. M808 forms a covalent bond between its acrylamide and the sulfur atom of Cys329 in menin[1]. |
| In Vivo | M-808 (16) is well tolerated in severe combined immunodeficiency (SCID) mice with intravenous administration of 10 mg/kg (or 25 mg/kg) every other day dosing (three times a week) for one week. M-808 (25 mg/kg) achieves a maximum tumor growth inhibition (TGI) of 97% during treatment (day 35) and reduces the average tumor volume from 92 mm3 at the beginning of the treatment to 59 mm3 at day 35, with no significant toxicity[1]. |
| References |
| Molecular Formula | C45H63FN6O5S |
|---|---|
| Molecular Weight | 819.08 |